AR119753A1 - Agonistas no peptídicos del receptor de la somatostatina tipo 5 y usos de los mismos - Google Patents

Agonistas no peptídicos del receptor de la somatostatina tipo 5 y usos de los mismos

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Publication number
AR119753A1
AR119753A1 ARP200102284A ARP200102284A AR119753A1 AR 119753 A1 AR119753 A1 AR 119753A1 AR P200102284 A ARP200102284 A AR P200102284A AR P200102284 A ARP200102284 A AR P200102284A AR 119753 A1 AR119753 A1 AR 119753A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
fluoroalkyl
alkyl
heteroalkyl
Prior art date
Application number
ARP200102284A
Other languages
English (en)
Inventor
Jian Zhao
Yunfei Zhu
Shimiao Wang
Mi Chen
Joseph Pontillo
Original Assignee
Crinetics Pharmaceuticals Inc
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Publication date
Application filed by Crinetics Pharmaceuticals Inc filed Critical Crinetics Pharmaceuticals Inc
Publication of AR119753A1 publication Critical patent/AR119753A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Endocrinology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1), o una sal o solvato del mismo aceptable desde el punto de vista farmacéutico, caracterizado porque: el Anillo A es carbociclo o heterociclo; X es N o C-Rᵃ; Y es N o C-Rᵇ; Z es N o C-Rᶜ; Rᵃ, Rᵇ, y Rᶜ son cada uno independientemente hidrógeno, halógeno, -CN, -N(R⁹)₂, -ORᶠ, -CO₂R⁹, -C(=O)N(R⁹)₂, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, fluoroalcoxi C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, carbociclo monocíclico sustituido o no sustituido, o heterociclo monocíclico sustituido o no sustituido; Rᶠ es -L¹-Rᵍ; L¹ está ausente, es alquileno C₁₋₆, fluoroalquileno C₁₋₆, o heteroalquileno C₁₋₆; Rᵍ es hidrógeno, cicloalquilo C₃₋₆ sustituido o no sustituido, fenilo sustituido o no sustituido, -CO₂R⁹, o -C(=O)N(R⁹)₂, heterociclo monocíclico sustituido o no sustituido; R¹ y R² son independientemente hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, cicloalquilo C₃₋₆ sustituido o no sustituido, o heterocicloalquilo C₃₋₅ sustituido o no sustituido; R³ es hidrógeno, -CN, -CO₂R⁹, -C(=O)N(R⁹)₂, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, alcoxi C₁₋₆ sustituido o no sustituido, fluoroalcoxi C₁₋₆ sustituido o no sustituido, o heteroalquilo C₁₋₆ sustituido o no sustituido; R⁴ y R⁵ son cada uno independientemente hidrógeno, halógeno, -OR⁹, -N(R⁹)₂, -CN, -CO₂R⁹, -C(=O)N(R⁹)₂, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, alcoxi C₁₋₆ sustituido o no sustituido, fluoroalcoxi C₁₋₆ sustituido o no sustituido, o heteroalquilo C₁₋₆ sustituido o no sustituido; R⁶ es alquilo C₁₋₈ sustituido o no sustituido, fluoroalquilo C₁₋₈ sustituido o no sustituido, heteroalquilo C₁₋₈ sustituido o no sustituido, o -L²-R⁶ᵃ; L² está ausente, es alquileno C₁₋₈ sustituido o no sustituido, o -CHR⁶ᵇ-; R⁶ᵃ es cicloalquilo C₃₋₁₀ sustituido o no sustituido, arilo C₆₋₁₀ sustituido o no sustituido, heterocicloalquilo C₂₋₁₀ sustituido o no sustituido, o heteroarilo C₁₋₉ sustituido o no sustituido; R⁶ᵇ es hidrógeno, alquilo C₁₋₆, fluoroalquilo C₁₋₆, o cicloalquilo C₃₋₆ sustituido o no sustituido; R⁷ es hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, cicloalquilo C₃₋₁₀ sustituido o no sustituido, arilo C₆₋₁₀ sustituido o no sustituido, heterocicloalquilo C₂₋₁₀ sustituido o no sustituido, o heteroarilo C₁₋₉ sustituido o no sustituido; o R⁶ y R⁷ se toman junto con el nitrógeno al cual ellos están enlazados a fin de formar un heterociclo que contiene N sustituido o no sustituido; cada R⁸, R¹¹, y R¹² es independientemente hidrógeno, halógeno, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, carbociclo monocíclico sustituido o no sustituido, heterociclo monocíclico sustituido o no sustituido, -CN, -OR⁹, -C(=O)R¹⁰, -CO₂R⁹, -C(=O)N(R⁹)₂, -N(R⁹)₂, -NR⁹C(=O)R¹⁰, -NR⁹C(=O)OR¹⁰, -NR⁹C(=O)N(R⁹)₂, -C(R⁹)=N-OR⁹, -SR⁹, -S(=O)R⁹, -SO₂R⁹, o -SO₂N(R⁹)₂; o R¹¹ se toma junto con un R⁸ adyacente y los átomos enlazan el R¹¹ y el R⁸ adyacente a fin de formar un carbociclo fusionado sustituido o no sustituido, o un heterociclo fusionado sustituido o no sustituido; cada R⁹ es independientemente hidrógeno, alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, cicloalquilo C₃₋₇ sustituido o no sustituido, heterocicloalquilo monocíclico de 3 a 8 elementos sustituido o no sustituido, fenilo sustituido o no sustituido, y heteroarilo monocíclico sustituido o no sustituido; o dos R⁹ en el mismo átomo N se toman junto con el átomo N al cual ellos están enlazados a fin de formar un heterociclo que contiene N sustituido o no sustituido; cada R¹⁰ es independientemente alquilo C₁₋₆ sustituido o no sustituido, fluoroalquilo C₁₋₆ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, cicloalquilo C₃₋₇ sustituido o no sustituido, heterocicloalquilo monocíclico de 3 a 8 elementos sustituido o no sustituido, fenilo sustituido o no sustituido, y heteroarilo monocíclico sustituido o no sustituido; y n es de 0 a 3.
ARP200102284A 2019-08-14 2020-08-12 Agonistas no peptídicos del receptor de la somatostatina tipo 5 y usos de los mismos AR119753A1 (es)

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US (2) US11479540B2 (es)
EP (1) EP4013748A4 (es)
JP (1) JP2022544055A (es)
KR (1) KR20220047318A (es)
CN (1) CN114585614A (es)
AR (1) AR119753A1 (es)
AU (1) AU2020327950A1 (es)
BR (1) BR112022002683A2 (es)
CA (1) CA3149840A1 (es)
CL (1) CL2022000354A1 (es)
CO (1) CO2022002781A2 (es)
IL (1) IL290479A (es)
MX (1) MX2022001874A (es)
PE (1) PE20221402A1 (es)
WO (1) WO2021030262A1 (es)
ZA (1) ZA202201829B (es)

Families Citing this family (10)

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MA51840A (fr) 2018-02-12 2021-05-19 Crinetics Pharmaceuticals Inc Modulateurs de somatostatine et leurs utilisations
EP3853218A4 (en) 2018-09-18 2022-02-16 Crinetics Pharmaceuticals, Inc. SOMATOSTATIN MODULATORS AND USES THEREOF
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KR20220047318A (ko) 2022-04-15
WO2021030262A1 (en) 2021-02-18
US11479540B2 (en) 2022-10-25
IL290479A (en) 2022-04-01
PE20221402A1 (es) 2022-09-15
JP2022544055A (ja) 2022-10-17
ZA202201829B (en) 2023-07-26
AU2020327950A1 (en) 2022-03-17
CL2022000354A1 (es) 2022-10-21
CA3149840A1 (en) 2021-02-18
CO2022002781A2 (es) 2022-06-21
EP4013748A4 (en) 2023-08-09
TW202115008A (zh) 2021-04-16
BR112022002683A2 (pt) 2022-07-05
US20220144802A1 (en) 2022-05-12
US20210047287A1 (en) 2021-02-18
CN114585614A (zh) 2022-06-03
EP4013748A1 (en) 2022-06-22
MX2022001874A (es) 2022-03-11

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